Cat. No.: HY-13298

Mps1-IN-1

5 Cited Publications

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Based on 5 publication(s) in Google Scholar

Mps1-IN-1 is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC₅₀ and a K_d of 367 nM and 27 nM.

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Pureté: 99.77%
CAS No.: 1125593-20-5
Formule: C₂₈H₃₃N₅O₄S
Masse moléculaire:535.66

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Mps1-IN-1 Chemical Structure

CAS No.: 1125593-20-5

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (5)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Mps1-IN-1 is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC₅₀ and a K_d of 367 nM and 27 nM^[1].

IC₅₀ & Target^[1]

Mps1

367 nM (IC₅₀)

Mps1

27 nM (Kd)

ALK

21 nM (Kd)

LTK

29 nM (Kd)

PYK2

280 nM (Kd)

FAK

440 nM (Kd)

IGF1R

750 nM (Kd)

INSR

470 nM (Kd)

CLK1

1900 nM (Kd)

ERK2

2900 nM (Kd)

INSRR

1200 nM (Kd)

TNK1

2600 nM (Kd)

TNK2

3100 nM (Kd)

GAK

1100 nM (Kd)

Cellular Effect

Cell Line	Type	Value	Description	References
AU565	IC₅₀	>10 μM Compound: Mps1-IN-1	Antiproliferative activity against human AU565 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay Antiproliferative activity against human AU565 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay	[PMID: 28259529]
BT-20	IC₅₀	>10 μM Compound: Mps1-IN-1	Antiproliferative activity against human BT20 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay Antiproliferative activity against human BT20 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay	[PMID: 28259529]
BT-474	IC₅₀	>10 μM Compound: Mps1-IN-1	Antiproliferative activity against human BT474 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay Antiproliferative activity against human BT474 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay	[PMID: 28259529]
BT-549	IC₅₀	1.73 μM Compound: Mps1-IN-1	Antiproliferative activity against human BT549 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay Antiproliferative activity against human BT549 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay	[PMID: 28259529]
CAL-51	IC₅₀	2.92 μM Compound: Mps1-IN-1	Antiproliferative activity against human CAL51 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay Antiproliferative activity against human CAL51 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay	[PMID: 28259529]
CAMA-1	IC₅₀	>10 μM Compound: Mps1-IN-1	Antiproliferative activity against human CAMA1 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay Antiproliferative activity against human CAMA1 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay	[PMID: 28259529]
HCC1937	IC₅₀	>10 μM Compound: Mps1-IN-1	Antiproliferative activity against human HCC1937 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay Antiproliferative activity against human HCC1937 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay	[PMID: 28259529]
Hs-578T	IC₅₀	>10 μM Compound: Mps1-IN-1	Antiproliferative activity against human Hs578T cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay Antiproliferative activity against human Hs578T cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay	[PMID: 28259529]
MCF7	IC₅₀	>10 μM Compound: Mps1-IN-1	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay	[PMID: 28259529]
MDA-MB-231	IC₅₀	>10 μM Compound: Mps1-IN-1	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay	[PMID: 28259529]
MDA-MB-436	IC₅₀	>10 μM Compound: Mps1-IN-1	Antiproliferative activity against human MDA-MB-436 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay Antiproliferative activity against human MDA-MB-436 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay	[PMID: 28259529]
MDA-MB-453	IC₅₀	>10 μM Compound: Mps1-IN-1	Antiproliferative activity against human MDA-MB-453 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay Antiproliferative activity against human MDA-MB-453 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay	[PMID: 28259529]
MDA-MB-468	IC₅₀	1.85 μM Compound: Mps1-IN-1	Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay Antiproliferative activity against human MDA-MB-468 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay	[PMID: 28259529]
SK-BR-3	IC₅₀	>10 μM Compound: Mps1-IN-1	Antiproliferative activity against human SK-BR-3 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay Antiproliferative activity against human SK-BR-3 cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay	[PMID: 28259529]
T47D	IC₅₀	>10 μM Compound: Mps1-IN-1	Antiproliferative activity against human T47D cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay Antiproliferative activity against human T47D cells assessed as reduction in cell viability after 5 to 7 days by CellTiter 96 aqueous solution assay	[PMID: 28259529]

In Vitro

Mps1-IN-1 is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC₅₀ and a K_d of 367 nM and 27 nM. Mps1-IN-1 also has high affinity for ALK, and LTK, with K_ds of 21 and 39 nM, respectively, but shows little or no inhibition on other 352 member kinases. Mps1-IN-1 (5, 10 μM) induces bypass of a checkpoint-mediated mitotic arrest in U2OS cells. Mps1-IN-1 disrupts recruitment of Mad2 to kinetochores, and reduces the phosphorylation status of Aurora B at threonine-232 (Thr232). Mps1-IN-1 (10 μM) shows no effect on centrosome duplication. In addition, Mps1-IN-1 (5-10 μM) suppresses the proliferative capacity of HCT116^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 1125593-20-5
Appearance Solid
Masse moléculaire 535.66
Formule C₂₈H₃₃N₅O₄S
Color Light yellow to yellow
SMILES

O=S(C(C=CC=C1)=C1NC2=CC(NC3=C(OC)C=C(N4CCC(O)CC4)C=C3)=NC5=C2C=CN5)(C(C)C)=O
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (5)

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Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
J Cancer

Proline-rich acidic protein 1 upregulates mitotic arrest deficient 1 to promote cisplatin-resistance of colorectal carcinoma by restraining mitotic checkpoint complex assembly. [Abstract]

2023 May 21;14(9):1515-1530. PMID: 37325046
Mol Reprod Dev

Phospholipase D2 Regulates Microtubule Acetylation by Modulating Gsk3β-Tau Signaling in Mouse Oocytes During Meiotic Maturation. [Abstract]

2025 Aug;92(8):e70051. PMID: 40838360
J Cell Biochem

Mps1 controls spindle assembly, SAC, and DNA repair in the first cleavage of mouse early embryos. [Abstract]

2021 Feb;122(2):290-300. PMID: 33025669
bioRxiv

2021 Feb 26.

Solvant et solubilité

In Vitro:

DMSO : ≥ 39 mg/mL (72.81 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8669 mL

9.3343 mL

18.6686 mL

5 mM

0.3734 mL

1.8669 mL

3.7337 mL

10 mM

0.1867 mL

0.9334 mL

1.8669 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.67 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

Kinase Assay^[1]

The kinase binding assay is used to assess compound binding to TTK by monitoring displacement of a fluorescently labeled, ATP site-directed kinase inhibitor (Kinase Tracer 236) from the kinase active site. Each 15 μL assay contains 5 nM TTK, variable amounts of test compound (Mps1-IN-1), 30 nM Kinase Tracer 236, 2 nM Eu-anti-GST Antibody, and 1% DMSO (residual from compound dilution) in Kinase Buffer A (50 mM HEPES pH 7.5, 10 mM MgCl₂, 1 mM EGTA, 0.01% Brij-35). Binding assays are initiated by addition of 5 μL of test compound (from 2-fold dilution series) to 5 μL of a kinase/antibody mixture, followed by addition of 5 μL of antibody. Assay plates are read using using standard Eu-based TR-FRET settings with excitation at 340 nm and emission monitored at 615 nm (donor) and 665 nm (acceptor). Emission intensities are measured over a 200 µs window following a 100 µs post-excitation delay^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[1]

U2OS cells expressing doxycycline-inducible PLK4 are plated in 96 well plates. A double thymidine block is performed using the following treatment regimen: thymidine for 18-20 hrs., release for 10 hrs. with doxycycline induction of PLK4 during this time, then a second thymidine block, followed by release. Six hours after the 2nd thymidine release, Mps1-IN-1 (or DMSO vehicle) is added and the proliferation of the cell populations is monitored with Cell Titer GLO assay^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (280 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Kwiatkowski N, et al. Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function. Nat Chem Biol. 2010 May;6(5):359-68. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8669 mL	9.3343 mL	18.6686 mL	46.6714 mL
	5 mM	0.3734 mL	1.8669 mL	3.7337 mL	9.3343 mL
	10 mM	0.1867 mL	0.9334 mL	1.8669 mL	4.6671 mL
	15 mM	0.1245 mL	0.6223 mL	1.2446 mL	3.1114 mL
	20 mM	0.0933 mL	0.4667 mL	0.9334 mL	2.3336 mL
	25 mM	0.0747 mL	0.3734 mL	0.7467 mL	1.8669 mL
	30 mM	0.0622 mL	0.3111 mL	0.6223 mL	1.5557 mL
	40 mM	0.0467 mL	0.2334 mL	0.4667 mL	1.1668 mL
	50 mM	0.0373 mL	0.1867 mL	0.3734 mL	0.9334 mL
	60 mM	0.0311 mL	0.1556 mL	0.3111 mL	0.7779 mL

Keywords

Mps1-IN-1

5 Cited Publications

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Mps1-IN-1

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Chemical Probe Library

Targeted Diversity Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Mps1-IN-1

Activité biologique

Chemical Information

Publications (5)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Mps1-IN-1

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Chemical Probe Library

Targeted Diversity Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Mps1-IN-1

Activité biologique

Chemical Information

Publications (5)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Mps1-IN-1 Related Classifications

HY-13298 Related Classifications